Drug intelligence / Profile preview

LOP628

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

LOP628 is an investigational antibody-drug conjugate (ADC) developed by Novartis. It consists of a humanized monoclonal IgG1/κ antibody targeting the stem cell factor receptor c-Kit (also known as proto-oncogene protein c-kit), conjugated via a non-cleavable linker to the cytotoxic agent maytansine. The mechanism of action involves specific binding to c-Kit-expressing tumor cells, internalization of the ADC, and intracellular release of maytansine, which inhibits tubulin polymerization and disrupts mitosis, leading to apoptosis in targeted cancer cells. LOP628 was primarily investigated for use in acute myeloid leukemia and solid tumors with overexpression or mutation of c-Kit[1][2][4][5][7].

Other names
Anti-c-kit humanised IgG1/κ antibody-maytansine conjugateAnti-proto-oncogene protein c-kit IgG1/kappa antibody-maytansine conjugate
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))

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